Table of Contents

1
1. Description: ................................................................................................................. 2
Generic name: ................................................................................................................... 2
Brand name: ...................................................................................................................... 2
Chemical name: ................................................................................................................ 2
Mechanism of action: ........................................................................................................ 2
Indications: ....................................................................................................................... 2
2. Stages of drug study design:........................................................................................ 2
2.1 Target identification: .................................................................................................... 2
2.2 Lead compound identification: .................................................................................... 2
2.3 Lead optimization: ....................................................................................................... 2
2.4 Pre-clinical evaluation:............................................................................................ 2
2.4.1 Chemistry: ............................................................................................................ 2
2.4.2 ADME parameters: ............................................................................................... 3
2.5 Clinical studies: ...................................................................................................... 3
2.6 Preformulating Studies: ............................................................................................... 3
Solubility: ..................................................................................................................... 3
Stability: ........................................................................................................................ 3
Particle size: .................................................................................................................. 3
Polymorphism: .............................................................................................................. 3
Excipient compatibility: ................................................................................................ 3
Drug-excipient interactions............................................................................................ 4
Physical characterization: ........................................................................................... 4
2.7 Product Formulations: ................................................................................................. 4
2.7.1 Excipients: ............................................................................................................ 4
2.8 Quality Control Tests For Alprazolam Tablets:............................................................. 4
2.8.1 Active Pharmaceutical Ingredient (API): ............................................................... 4
2.8.2 Excipients: ............................................................................................................ 4
2.9 New Drug Application ................................................................................................. 4
2.10 Post-Marketing Surveillance ...................................................................................... 4
3. References:................................................................................................................... 5
 Alprazolam

1. Description:
Alprazolam was invented by Jackson Hester Jr. at the Upjohn Company and patented in 1971
and approved for medical use in the United States in 1981. Alprazolam is a Schedule IV
controlled substance and is a common drug of abuse. Alprazolam is a triazolo analog of the 1,4
benzodiazepine class of central nervous system-active compounds.

Generic name: Alprazolam

Brand name: Alap
Chemical name: 8-Chloro-1-methyl-6-phenyl-4H-s-triazolo [4,3-α] [1,4] benzodiazepine
Mechanism of action:
Alprazolam enhances the effects of gamma-aminobutyric acid (GABA) neurotransmitters,
leading to a calming effect on the central nervous system.
Indications:
Alprazolam is indicated for anxiety disorders, panic disorder with or without agoraphobia,
Anxiety associated with depression

2. Stages of drug study design:

2.1 Target identification:
Alprazolam primarily targets and enhances the function of GABA-A receptors, specifically
subunits α1, α2, α3, and α5, leading to its anxiolytic and sedative effects in the central nervous
system.
2.2 Lead compound identification:
Alprazolam identified as a lead compound
2.3 Lead optimization:
Refinement of Alprazolam's chemical structure and pharmacological properties for improved
efficacy and reduced side effects.
2.4 Pre-clinical evaluation:
2.4.1 Chemistry:
Chemical formula: C17H13ClN4
Molar mass: 308.765 g/mol
Structural formula:

2.4.2 ADME parameters:

Absorption:
Following oral administration, alprazolam is readily absorbed Approximately 11–12.5 hours
for immediate-release preparations; approximately 11–16 hours for extended-release tablets.
Distribution:
In vitro, alprazolam is bound (80 percent) to human serum protein. Serum albumin accounts
for the majority of the binding.
Metabolism:
Extensively metabolized in the liver by CYP3A4 to metabolites that are inactive or have
lower potency than alprazolam.
Elimination:
Alprazolam and metabolites are excreted primarily in urine.
2.5 Clinical studies:
Clinical studies on Alprazolam have scrutinized its efficacy and safety in managing anxiety
disorders and panic attacks, typically through randomized controlled trials comparing it with
placebos or alternative medications. These trials evaluate symptom reduction, quality of life
enhancements, and the occurrence of adverse effects like dependency and withdrawal.
2.6 Preformulating Studies:
Evaluation of physical and chemical properties of Alprazolam for formulation development.
Solubility: It is refers to how well alprazolam dissolves in different solvents
Stability: Stability studies assess how alprazolam degrades over time under different
conditions such as temperature, humidity, and light exposure. This information helps design
packaging and storage conditions to maintain the drug's potency and shelf-life.

Particle size: Particle size affects the drug's dissolution rate, bioavailability, and stability.

Polymorphism: Alprazolam may exist in different crystalline forms (polymorphs), which can
influence its solubility, stability, and bioavailability. Characterizing the polymorphic forms
helps select the most suitable form for formulation and ensures product consistency.

Excipient compatibility: Compatibility studies evaluate the interactions between alprazolam

and various excipients used in formulations, such as binders, disintegrants, and lubricants.
Identifying compatible excipients ensures formulation stability and effectiveness.
Drug-excipient interactions: Beyond compatibility, it's important to assess any potential
chemical or physical interactions between alprazolam and excipients that could affect the drug's
stability, efficacy, or safety.

Physical characterization: This involves techniques like differential scanning calorimetry

(DSC), X-ray diffraction (XRD), and microscopy to characterize the physical properties of
alprazolam, including its crystallinity, morphology, and melting behavior.

2.7 Product Formulations:

2.7.1 Excipients:
 Docusate sodium
 Lactose monohydrate
 Magnesium stearate
 Cellulose, microcrystalline
 Starch, corn
 Sodium benzoate
2.8 Quality Control Tests For Alprazolam Tablets:
2.8.1 Active Pharmaceutical Ingredient (API):
Purity, potency, and stability testing of Alprazolam.
2.8.2 Excipients:
 Identification
 purity
 Moisture content
 pH
 Heavy metals
2.8.3 In -process QC test:
 Appearance and physical characteristics
 Content uniformity
 Dissolution test
 Disintegration
 Assay
 Weight variation
2.9 New Drug Application
Submission of comprehensive data to regulatory authorities for Alprazolam's approval as a new
drug.
2.10 Post-Marketing Surveillance
Monitoring adverse events, efficacy, and safety of Alprazolam after-market release
3. References:
 United state pharmacopeia (USP)/Alprazolam monograph.org.com
 DrugBank.com